AR082076A2 - Succinato de o-desmetil-venlafaxina, composicion farmaceutica que lo comprende, forma de dosificacion que lo comprende, su uso en la manufactura de un medicamento, y metodo para prepararlo - Google Patents
Succinato de o-desmetil-venlafaxina, composicion farmaceutica que lo comprende, forma de dosificacion que lo comprende, su uso en la manufactura de un medicamento, y metodo para prepararloInfo
- Publication number
- AR082076A2 AR082076A2 ARP110102372A ARP110102372A AR082076A2 AR 082076 A2 AR082076 A2 AR 082076A2 AR P110102372 A ARP110102372 A AR P110102372A AR P110102372 A ARP110102372 A AR P110102372A AR 082076 A2 AR082076 A2 AR 082076A2
- Authority
- AR
- Argentina
- Prior art keywords
- venlafaxine
- desmethyl
- disorder
- crystalline
- understands
- Prior art date
Links
- 239000002552 dosage form Substances 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 229960004688 venlafaxine Drugs 0.000 title abstract 2
- 229940126601 medicinal product Drugs 0.000 title 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 title 1
- ORUUBRMVQCKYHB-UHFFFAOYSA-N butanedioic acid;4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol Chemical compound OC(=O)CCC(O)=O.C1CCCCC1(O)C(CN(C)C)C1=CC=C(O)C=C1 ORUUBRMVQCKYHB-UHFFFAOYSA-N 0.000 abstract 6
- KYYIDSXMWOZKMP-UHFFFAOYSA-N O-desmethylvenlafaxine Chemical compound C1CCCCC1(O)C(CN(C)C)C1=CC=C(O)C=C1 KYYIDSXMWOZKMP-UHFFFAOYSA-N 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000000994 depressogenic effect Effects 0.000 abstract 2
- 239000003937 drug carrier Substances 0.000 abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 2
- 201000000736 Amenorrhea Diseases 0.000 abstract 1
- 206010001928 Amenorrhoea Diseases 0.000 abstract 1
- 208000000103 Anorexia Nervosa Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 abstract 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 abstract 1
- 206010003805 Autism Diseases 0.000 abstract 1
- 208000020706 Autistic disease Diseases 0.000 abstract 1
- 206010006550 Bulimia nervosa Diseases 0.000 abstract 1
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 206010012335 Dependence Diseases 0.000 abstract 1
- 208000020401 Depressive disease Diseases 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 1
- 208000001640 Fibromyalgia Diseases 0.000 abstract 1
- 208000011688 Generalised anxiety disease Diseases 0.000 abstract 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 abstract 1
- 208000001089 Multiple system atrophy Diseases 0.000 abstract 1
- 241000208125 Nicotiana Species 0.000 abstract 1
- 235000002637 Nicotiana tabacum Nutrition 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 abstract 1
- 208000003782 Raynaud disease Diseases 0.000 abstract 1
- 208000012322 Raynaud phenomenon Diseases 0.000 abstract 1
- 201000001880 Sexual dysfunction Diseases 0.000 abstract 1
- 208000009106 Shy-Drager Syndrome Diseases 0.000 abstract 1
- 206010041250 Social phobia Diseases 0.000 abstract 1
- 208000000323 Tourette Syndrome Diseases 0.000 abstract 1
- 208000016620 Tourette disease Diseases 0.000 abstract 1
- 206010046543 Urinary incontinence Diseases 0.000 abstract 1
- 229910052783 alkali metal Inorganic materials 0.000 abstract 1
- -1 alkali metal salt Chemical class 0.000 abstract 1
- 231100000540 amenorrhea Toxicity 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 abstract 1
- 208000030963 borderline personality disease Diseases 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 229960003920 cocaine Drugs 0.000 abstract 1
- 230000019771 cognition Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 230000017858 demethylation Effects 0.000 abstract 1
- 238000010520 demethylation reaction Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 208000029364 generalized anxiety disease Diseases 0.000 abstract 1
- 230000002267 hypothalamic effect Effects 0.000 abstract 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 abstract 1
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 208000019906 panic disease Diseases 0.000 abstract 1
- 208000028173 post-traumatic stress disease Diseases 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 231100000872 sexual dysfunction Toxicity 0.000 abstract 1
- 230000000391 smoking effect Effects 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 230000001457 vasomotor Effects 0.000 abstract 1
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/10—Succinic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/20—Hypnotics; Sedatives
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/64—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Emergency Medicine (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Se provee una sal de la O-desmetil venlafaxina, el succinato de O-desmetilvenlafaxina. También se proveen composiciones farmacéuticas, formas de dosificación, métodos para prepararla y usos de la misma.Reivindicación 7: Un compuesto de la reivindicación 6, caracterizado porque el compuesto exhibe un patrón de difracción de Rayos X de polvo que tiene picos característicos expresados en grados 2q (± 0,2º 2q) a 10,36, 13,74, 14,40, 14,68, 14,96, 16,75, 17,48, 17,76, 19,26, 20,42, 20,74, 22,55, 23,58, 23,82, 24,92, 26,00, 31,86 y 32,42. Reivindicación 11: Una composición farmacéutica caracterizada porque comprende succinato de O-desmetil venlafaxina cristalino según cualquiera de las reivindicaciones 1 a 10 y un vehículo o excipiente farmacéuticamente aceptable. Reivindicación 13: Una forma de dosificación farmacéutica caracterizada porque comprende una cantidad terapéuticamente efectiva de succinato de O-desmetil venlafaxina cristalino según cualquiera de las reivindicaciones 1 a 10 y un vehículo o excipiente farmacéuticamente aceptable. Reivindicación 23: Uso del succinato de O-desmetil-venlafaxina cristalino según cualquiera de las reivindicaciones 1 a 10 caracterizado porque es en la manufactura de un medicamento para (i) el tratamiento de depresión, ansiedad, trastorno de pánico, trastorno de ansiedad generalizada, trastorno de estrés post-traumático, fibromialgia, agorofobia, trastorno de déficit de atención, trastorno compulsivo obsesivo, trastorno de ansiedad social, autismo, esquizofrenia, obesidad, anorexia nerviosa, bulimia nerviosa, Síndrome de Gilles de la Tourette, rubor vasomotor, adicción a la cocaína y al alcohol, disfunción sexual, trastorno de personalidad fronteriza, síndrome de fatiga crónica, incontinencia urinaria, dolor, síndrome de Shy Drager, síndrome de Raynaud, enfermedad de Parkinson y epilepsia en un paciente; (ii) mejorar la cognición o tratar el deterioro cognitivo en un paciente; (iii) dejar de fumar u otros usos del tabaco en un paciente; (iv) tratar el desorden disfórico premenstrual en una mujer o la amenorrea hipotalámica en una mujer deprimida o no deprimida. Reivindicación 24: Un método para preparar succinato de O-desmetil-venlafaxina cristalino de acuerdo con la reivindicación 1, caracterizado porque comprende los pasos de: (a) desmetilación de venlafaxina o una sal de la misma con una sal de metal alcalino de un trialquil borohidruro para dar O-desmetil-venlafaxina; y (b) conversión de O-desmetil-venlafaxina en succinato de O-desmetil-venlafaxina; y (c) cristalizar directamente la sal cristalina a partir de un solvente.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26821401P | 2001-02-12 | 2001-02-12 | |
| US29796301P | 2001-06-13 | 2001-06-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR082076A2 true AR082076A2 (es) | 2012-11-07 |
Family
ID=26952945
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020100463A AR032671A1 (es) | 2001-02-12 | 2002-02-12 | Succinato novedoso de la o-desmetilvenlafaxina |
| ARP110102372A AR082076A2 (es) | 2001-02-12 | 2011-07-01 | Succinato de o-desmetil-venlafaxina, composicion farmaceutica que lo comprende, forma de dosificacion que lo comprende, su uso en la manufactura de un medicamento, y metodo para prepararlo |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020100463A AR032671A1 (es) | 2001-02-12 | 2002-02-12 | Succinato novedoso de la o-desmetilvenlafaxina |
Country Status (30)
| Country | Link |
|---|---|
| US (5) | US6673838B2 (es) |
| EP (3) | EP2319826A1 (es) |
| JP (1) | JP4220243B2 (es) |
| KR (1) | KR100875610B1 (es) |
| CN (2) | CN101671260A (es) |
| AR (2) | AR032671A1 (es) |
| AT (1) | ATE369330T1 (es) |
| AU (1) | AU2002250058B2 (es) |
| BR (1) | BR0207157A (es) |
| CA (2) | CA2666611A1 (es) |
| CY (1) | CY1106952T1 (es) |
| DE (1) | DE60221642T3 (es) |
| DK (1) | DK1360169T3 (es) |
| EA (1) | EA011451B1 (es) |
| ES (1) | ES2290281T5 (es) |
| HN (1) | HN2002000030A (es) |
| HU (1) | HUP0303128A3 (es) |
| IL (4) | IL157340A0 (es) |
| MX (1) | MXPA03007043A (es) |
| NO (1) | NO328807B1 (es) |
| NZ (1) | NZ539791A (es) |
| PA (1) | PA8539901A1 (es) |
| PE (1) | PE20020877A1 (es) |
| PL (2) | PL211788B1 (es) |
| PT (1) | PT1360169E (es) |
| SI (1) | SI1360169T1 (es) |
| TW (1) | TWI318201B (es) |
| UY (1) | UY27175A1 (es) |
| WO (1) | WO2002064543A2 (es) |
| ZA (1) | ZA200307116B (es) |
Families Citing this family (115)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2348021A1 (en) | 1998-10-30 | 2000-05-11 | Ajinomoto Co., Inc. | Crystallization processes for the formation of stable crystals of aspartame derivative |
| US6342533B1 (en) | 1998-12-01 | 2002-01-29 | Sepracor, Inc. | Derivatives of (−)-venlafaxine and methods of preparing and using the same |
| HUP0200898A3 (en) * | 1999-04-06 | 2005-09-28 | Sepracor Inc | Derivatives of venlafaxine and methods of preparing and using the same |
| EP2319826A1 (en) * | 2001-02-12 | 2011-05-11 | Wyeth LLC | Succinate salt of O-desmethyl-venlafaxin |
| US20050244498A1 (en) * | 2001-09-14 | 2005-11-03 | Biovail Laboratories, Inc. | Modified-release compositions of at least one form of venlafaxine |
| UA80543C2 (en) | 2001-12-04 | 2007-10-10 | Wyeth Corp | Method for the preparation of o-desmethylvenlafaxine |
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